4.5 Article

Tetraphenylethylene-Based Photoluminescent Self-Assembled Nanoparticles: Preparation and Biological Evaluation

Journal

ACS MEDICINAL CHEMISTRY LETTERS
Volume 14, Issue 10, Pages 1472-1477

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.3c00396

Keywords

Tetraphenylethylene; self-assemblednanoparticles; cancer cell lines; podophyllotoxin; N-desacetylthiocolchicine; cabazitaxel; aggregation-induced emission

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Fluorescent nanoparticles were formed by conjugating tetraphenylethylene (TPE) with podophyllotoxin, N-desacetyl-thiocolchicine, and cabazitaxel through a sebacic acid linker. The identification and characterization of the fluorescent nanoparticles were achieved using dynamic light scattering (DLS) and photoluminescence spectroscopy. The biological evaluation in various cancer cell lines showed that the nanoparticles maintained the activity of cabazitaxel and exhibited high blue fluorescence. The internalization of the fluorescent nanoparticles into cells was confirmed using immunofluorescence assay.
The conjugation of tetraphenylethylene (TPE) with podophyllotoxin, N-desacetyl-thiocolchicine, and cabazitaxel through a sebacic acid linker led to the formation of fluorescent nanoparticles. Dynamic light scattering (DLS) and photoluminescence spectroscopy were used for the identification and characterization of the fluorescent nanoparticles. The biological evaluation was determined in three human ovarian (KURAMOCHI, OVCAR3, OVSAHO) and three human breast (MCF7, SKBR 3, and MDA-MB231) cancer cell lines. In the case of cabazitaxel, the nanoparticles maintained the activity of the parent drug, at the low nanomolar range, while exhibiting high blue fluorescence. The internalization of the fluorescent NPs into cells was detected using immunofluorescence assay.

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